Patent SG-11201906209S-A (SG)
Title: Bicyclic compounds as allosteric shp2 inhibitors
Inventor: KOLTUN ELENA S
IPC: C07D498/04
Filed: 2018-01-09
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 July 2018 (26.07.2018) WIPO I PCT omit IIl °nolo Oil IIIII Imo oimIE (10) International Publication Number WO 2018/136265 Al (51) International Patent Classification: CO7D 471/04 (2006.01) CO7D 519/00 (2006.01) CO7D 487/04 (2006.01) A61P 35/00 (2006.01) CO7D 491/048 (2006.01) A61K 31/437 (2006.01) CO7D 498/04 (2006.01) A61K 31/4375 (2006.01) CO7D 513/04 (2006.01) A61K 31/4985 (2006.01) (21) International Application Number: PCT/US2018/013023 (22) International Filing Date: 09 January 2018 (09.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/449,530 23 January 2017 (23.01.2017) US (71) Applicant: REVOLUTION MEDICINES, INC. [US/US]; 700 Saginaw Drive, Redwood City, California 94063 (US). (72) Inventors; and (71) Applicants: BLANK, Brian R. [US/US]; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, Cali- fornia 94063 (US). PITZEN, Jennifer [US/US]; c/o Revo- lution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). WANG, Gang [US/US]; c/o Revo- lution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). WON, Walter S. [US/US]; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). TZITZILONIS, Christos [US/US]; c/o Revolution Medicines, Inc., 700 Saginaw Dri- ve, Redwood City, California 94063 (US). LI, Jie Jack [US/US]; c/o Revolution Medicines, Inc., 700 Saginaw Dri- ve, Redwood City, California 94063 (US). (72) Inventors: KOLTUN, Elena S.; c/o Revolution Medi- cines, Inc., 700 Saginaw Drive, Redwood City, Califor- nia 94063 (US). AAY, Naing; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). BUCKL, Andreas; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). MELLEM, Kevin; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). SEMKO, Christopher; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). JOGALEKAR, Ash; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). KISS, Gert; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). GILL, Adri- an; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). (74) Agent: TONG, Connie C. et al.; Cooley LLP, 1299 Penn- sylvania Avenue, NW, Suite 700, Washington, District of Columbia 20004 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) O (57) : The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are 0 pharmaceutical compositions comprising the same. (54) Title: BICYCLIC COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS